Study on Biological Activity of Isoquinoline-Type Alkaloids

1.异喹啉生物碱的生物活性(1)原小檗碱型生物碱的细胞毒活性利用人癌细胞系和药敏数据库，对24个与黄连素相关的四元原小檗碱生物碱的细胞毒活性进行了评价。在第8位或第13位延伸烷基对细胞毒活性有很大影响，即相对亲脂性和取代基的大小影响细胞毒活性。(2)简单异喹啉和苄基异喹啉生物活性26个简单异喹啉和21个苄基异喹啉生物活性被检测为抗微生物、抗疟疾、细胞毒和抗HIV活性。一些简单的异喹啉生物碱在每一种测定中都具有显著的活性，可能作为开发潜在化疗药物的先导化合物。异喹啉型四元氮原子m-…在前三种类型的活动中，更多的可能有助于增强效力。与之相反，四氢异喹啉类化合物具有抗HIV活性。(3)黄连素相关生物碱的杀菌和除草活性。对23个与黄连素相关的季胺和叔胺类化合物进行了体外和/或体内的杀菌和除草活性测试。在被测试的化合物中，只有一些原小檗盐观察到了一些活性，但没有足够的强度或广谱用于农用化学用途。从结构-活动的角度来看，可以指出一些特点。延胡索属植物细胞培养中生物碱代谢产物的LC/核磁共振和LC/MS分析研究了1-苄基四氢异喹啉在延胡索属植物细胞中的生物转化。利用LC/MS和LC/核磁共振技术对代谢物进行鉴定。这些技术使我们能够快速地为这些代谢物指定结构，同时避免分离单独的化合物。一些代谢物是新的2，3，10，11-氧合原黄连素。较少

1. Biological Activity of Isoquinoline Alkaloids(1) Cytotoxicity of the Protoberberine-Type AlkaloidsCytotoxic activities of twenty four quaternary protoberberine alkaloids related to berberine have been evaluated using a human cancer cell line panel coupled with a drug sensitivity database. Extending the alkyl chain at position 8 or 13 strongly influenced the cytotoxic activity, that is, relative lipophilicity as well as the size of the substituent affects cytotoxicity. The highest level of activity was observed in 8- or 13-hexyl substituted derivatives of berberine.(2) Biological Activity of Simple Isoquinoline and Benzylisoquinoline AlkaloidsTwenty-six simple isoquinolines and 21 benzylisoquinolines were tested for antimicrobial, antimalarial, cytotoxic, and anti-HIV activities. Some simple isoquinoline alkaloids significantly active in each assay, and may be useful as lead compounds for developing potential chemotherapeutic agents. A quatemary nitrogen atom of isoquinolinium type m … More ay contribute to enhanced potency in the first three types activities. In contrast, anti-HIV activity was found with tetrahydroisoquinoline-type salts.(3) Fungicidal and Herbicidal Activities of Berberine Related AlkaloidsThe 23 quaternary and tertiary protoberberines related to berberine were tested for in vitro and/or in vivo fungicidal and herbicidal activities. Among the compounds tested, there was some activity observed with some of only the protoberberiniumsalts, but not sufficiently strong or broad spectrum for agrochemical utility. From the structure-activity point of view, some features can be pointed out.2. Structural Analysis of Alkaloid Metabolites in Cell Culture of Corydalis Species by LC/NMR and LC/MSThe biotransformations of 1-benzyltetrahydroisoquinolines in the cultured cells of Corydalis species were studied. Identification of metabolites was performed using LC/MS and LC/NMR techniques. These techniques enabled us to assign rapidly structures to these metabolites while avoiding the isolation of individual compounds. It was found that some metabolites were new 2, 3, 10, 11-oxygenated protoberberines. Less